Reaction Details Report a problem with these data
Target
Methionine aminopeptidase 2
Ligand
BDBM17362
Substrate
BDBM17353
Meas. Tech.
Enzyme Inhibition Assay
pH
7.5±n/a
Temperature
295.15±n/a K
Ki
0.15±n/a nM
Km
300000±n/a nM
Citation
Marino, JP; Fisher, PW; Hofmann, GA; Kirkpatrick, RB; Janson, CA; Johnson, RK; Ma, C; Mattern, M; Meek, TD; Ryan, MD; Schulz, C; Smith, WW; Tew, DG; Tomazek, TA; Veber, DF; Xiong, WC; Yamamoto, Y; Yamashita, K; Yang, G; Thompson, SK Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore. J Med Chem 50:3777-85 (2007) [PubMed] Article
Target
Name:
Methionine aminopeptidase 2
Synonyms:
Initiation factor 2-associated 67 kDa glycoprotein | MAP 2 | MAP2_HUMAN | METAP2 | MNPEP | MetAP 2 | Methionine aminopeptidase 2 (MetAP2) | Methionine aminopeptidases (HsMetAP2) | P67EIF2 | Peptidase M 2 | p67
Type:
Enzyme
Mol. Mass.:
52884.45
Organism:
Homo sapiens (Human)
Description:
P50579
Residue:
478
Sequence:
MAGVEEVAASGSHLNGDLDPDDREEGAASTAEEAAKKKRRKKKKSKGPSAAGEQEPDKESGASVDEVARQLERSALEDKERDEDDEDGDGDGDGATGKKKKKKKKKRGPKVQTDPPSVPICDLYPNGVFPKGQECEYPPTQDGRTAAWRTTSEEKKALDQASEEIWNDFREAAEAHRQVRKYVMSWIKPGMTMIEICEKLEDCSRKLIKENGLNAGLAFPTGCSLNNCAAHYTPNAGDTTVLQYDDICKIDFGTHISGRIIDCAFTVTFNPKYDTLLKAVKDATNTGIKCAGIDVRLCDVGEAIQEVMESYEVEIDGKTYQVKPIRNLNGHSIGQYRIHAGKTVPIVKGGEATRMEEGEVYAIETFGSTGKGVVHDDMECSHYMKNFDVGHVPIRLPRTKHLLNVINENFGTLAFCRRWLDRLGESKYLMALKNLCDLGIVDPYPPLCDIKGSYTAQFEHTILLRPTCKEVVSRGDDY
Inhibitor
Name:
BDBM17362
Synonyms:
1,2,4-Triazole Compound, 20 | 5-[(3-methylbut-2-en-1-yl)sulfanyl]-N-(2-methylphenyl)-4H-1,2,4-triazol-3-amine
Type:
Small organic molecule
Emp. Form.:
C14H18N4S
Mol. Mass.:
274.385
SMILES:
CC(C)=CCSc1nnc(Nc2ccccc2C)[nH]1 |(5.94,4.3,;4.59,5.03,;4.55,6.57,;3.28,4.22,;1.81,4.7,;.67,3.67,;-.8,4.15,;-1.27,5.61,;-2.81,5.61,;-3.29,4.15,;-4.75,3.67,;-5.9,4.7,;-5.13,6.03,;-5.9,7.37,;-7.44,7.37,;-8.21,6.03,;-7.44,4.7,;-8.21,3.37,;-2.04,3.24,)|